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81. 发明申请

US20030199580A1 Intermediates for the synthesis of benzimidazole derivatives and a process for the preparation thereof 失效
标题翻译：用于合成苯并咪唑衍生物的中间体及其制备方法
公开(公告)号：US20030199580A1
公开(公告)日：2003-10-23
申请号：US10272133
申请日：2002-10-16
申请人： SANKYO COMPANY, LIMITED
发明人： Naoyuki Kishi , Yoshitaka Nakamura , Narumi Abe , Toyonori Takebayashi
IPC分类号： C07C069/76 , A61K031/24 , A61K031/135
CPC分类号： C07C271/28 , C07D277/34 , C07D417/12 , Y02P20/55
摘要： This invention provides a process for the preparation of a benzimidazole derivative (I) or a pharmaceutically acceptable salt thereof, 1 wherein R1 is C1-C6 alkyl, C1-C6 alkoxyl, etc., R2 is C1-C6 alkyl, and R3 is hydrogen or a protecting group, which exhibits excellent hyopoglycemic action, said process comprising condensation of an amine derivative (III) with a carboxylic acid derivatives (II) to afford a compound (IV), followed by cyclization of compound (IV) in the presence of an acid.
摘要翻译：本发明提供了制备苯并咪唑衍生物（I）或其药学上可接受的盐的方法，其中R 1是C 1 -C 6烷基，C 1 -C 6烷氧基等，R 2是C 1 -C 6烷基，并且R 3是氢或保护基，其表现出优异的血压作用，所述方法包括将胺衍生物（III）与羧酸衍生物（II）缩合，得到化合物（IV），然后环化化合物（Ⅳ）在酸存在下反应。

82. 发明申请

US20030176364A1 Antimicrobial therapeutic compositions and methods of use 失效
标题翻译：抗微生物治疗组合物和使用方法
公开(公告)号：US20030176364A1
公开(公告)日：2003-09-18
申请号：US10370411
申请日：2003-02-18
发明人： Dusan Ninkov
IPC分类号： A61K031/7024 , A61K031/24 , A61K031/05
CPC分类号： A61K31/05 , A61K31/16 , A61K45/06 , A61K2300/00
摘要： The invention provides therapeutic antimicrobial compositions and methods for their use based on natural organic phenolic compounds combined with pharmacological agents. The antimicrobial activities of each carvacrol and thymol are believed to be enhanced, while the pharmacological properties of procaine and related compounds are added to provide their unique properties to facilitate usefulness and effectiveness in humans. The therapeutic compositions are active against bacterial, fungal, and protozoan infections. The forms of the invention are intended to treat various internal infections through parenteral, subcutaneous, intradermal, intravenous, and intramuscular injections. They are also intended as useful agents to treat microbial infections that have become resistant to conventional anitibiotics as well as secondary opportunistic infections.
摘要翻译：本发明提供治疗性抗微生物组合物及其基于天然有机酚类化合物与药物代谢物组合使用的方法。据信，每种香芹酚和百里酚的抗微生物活性得到增强，而普鲁卡因和相关化合物的药理学性质被加入以提供其独特的性质来促进人类的有用性和有效性。治疗组合物对细菌，真菌和原生动物感染具有活性。本发明的形式旨在通过肠胃外，皮下，皮内，静脉内和肌内注射治疗各种内部感染。它们也被用作治疗已经变得对常规的抗生素以及次级机会性感染具有抗性的微生物感染的有用试剂。

83. 发明申请

US20030166685A1 Acid derivatives useful as serine protease inhibitors 有权
标题翻译：用作丝氨酸蛋白酶抑制剂的酸衍生物
公开(公告)号：US20030166685A1
公开(公告)日：2003-09-04
申请号：US10052927
申请日：2001-11-07
发明人： Gregory S. Bisacchi , James C. Sutton , William A. Slusarchyk , Uwe D. Treuner , Guohua Zhao , Daniel L. Cheney , Yan Shi , Shung C. Wu
IPC分类号： A61K031/44 , A61K031/4439 , A61K031/24 , C07C229/54
CPC分类号： C07D401/12 , A61K45/06 , C07B2200/07 , C07C257/18 , C07D207/16 , C07D211/60 , C07D223/06
摘要： Compounds having the formula (I), 1 are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, IXa, Xa, and/or XIa, wherein ring B is phenyl or pyridyl, W is preferably C(nullO)NR4R5, L is a linker group, X2 comprises nitrogen or carbon, Z is an optionally-substituted monocyclic or bicyclic ring system, and R1, R2, R3, R4, R5 and R6 are as defined in the specification.
摘要翻译：具有式（I）的化合物可用作丝氨酸蛋白酶抑制剂，更具体地可用作因子VIIa，IXa，Xa和/或XIa的抑制剂，其中环B是苯基或吡啶基，W优选为C（= O）NR 4 R 5，L 是连接基团，X 2包括氮或碳，Z是任选取代的单环或双环环系，R1，R2，R3，R4，R5和R6如说明书中所定义。

84. 发明申请

US20030158253A1 Ethers of O-Desmethyl venlafaxine 审中-公开
标题翻译： O-去甲基文拉法辛的醚
公开(公告)号：US20030158253A1
公开(公告)日：2003-08-21
申请号：US10315699
申请日：2002-12-10
申请人： Wyeth
发明人： John P. Yardley , Magid A. Abou-Gharbia , John W. Ullrich
IPC分类号： C07D307/93 , A61K031/343 , A61K031/277 , C07C255/58 , C07C229/28 , A61K031/24
CPC分类号： C07C217/64 , C07C2601/14
摘要： This invention provides O-null-acyloxyalkyl ethers of the venlafaxine metabolite 4-null2-(Dimethylamino-1-(1-hydroxycyclohexyl)ethylnullphenol, represented by Formula (I): 1 wherein: the configuration at the steriogenic center (*) may be R, S, or RS (the racemate); R1 is selected from C1-C6 alkyl, C1-C6 alkoxy, C3-C6 cycloalkyl, or the moiety: 2 R2 is selected from H, or C1-C6 alkyl; or, R1 and R2 may be concatenated such that 3 nullform a moiety having formula (b): 4 R3 is selected from H or C1-C6 alkyl; and R4 and R5 are independently selected from H, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 thioalkoxy, nullCN, nullOH, nullCF3, nullOCF3, halogen, nullNH2, nullNO2, or mono or dialkylamino wherein each alkyl group has 1 to 6 carbon atoms, or pharmaceutically acceptable salts or hydrates thereof, R, S, or RS forms thereof; as well as pharmaceutical compositions and methods treating central nervous system disorders.
摘要翻译：本发明提供文拉法辛代谢物4- [2-（二甲基氨基-1-（1-羟基环己基）乙基]苯酚，由式（I）表示的O-α-酰氧基烷基醚：其中：在灭菌中心（*）可以是R，S或RS（外消旋体）; R 1选自C 1 -C 6烷基，C 1 -C 6烷氧基，C 3 -C 6环烷基或部分：R 2选自H或C 1 -C 6烷基; R 1和R 2可以连接形成具有式（b）的部分：R 3选自H或C 1 -C 6烷基; R 4和R 5独立地选自H，C 1 -C 6烷基，C 3 -C 6环烷基， C6烷氧基，C1-C6硫代烷氧基，-CN，-OH，-CF3，-OCF3，卤素，-NH2，-NO2，或其中每个烷基具有1至6个碳原子的单或二烷基氨基，或其药学上可接受的盐或水合物，R，S或RS形式;以及治疗中枢神经系统疾病的药物组合物和方法。

85. 发明申请

US20030134897A1 Aromatic compositions for the inhibition of exoprotein production from gram positive bacteria 失效
标题翻译：用于抑制革兰氏阳性细菌产生外源蛋白的芳香族组合物
公开(公告)号：US20030134897A1
公开(公告)日：2003-07-17
申请号：US09969218
申请日：2001-10-02
申请人： Kimberly-Clark Worldwide, Inc.
发明人： Rae Ellen Syverson , Richard A. Proctor
IPC分类号： A61K031/27 , A61K031/24
CPC分类号： A61L15/46 , A61L2300/402 , A61L2300/404 , A61L2300/41 , A61L2300/45 , A61L2300/802
摘要： Compositions including an aromatic compound for inhibiting the production of exoproteins by Gram positive bacteria are disclosed. The aromatic inhibitory compounds of the present invention have the general formula: 1 wherein R1 is selected from the group consisting of H, 2 nullOR5, nullR6C(O)H, nullR6OH, nullR6COOH, nullOR6OH, nullOR6COOH, nullC(O)NH2, 3 and NH2 and salts thereof; R5 is a monovalent saturated or unsaturated aliphatic hydrocarbyl moiety; R6 is a divalent saturated or unsaturated aliphatic hydrocarbyl moiety; R7 is a trivalent saturated or unsaturated aliphatic hydrocarbyl moiety; R8 is a monovalent substituted or unsubstituted saturated or unsaturated aliphatic hydrocarbyl moiety which may or may not be interrupted with hetero atoms; R2, R3, and R4 are independently selected from the group consisting of H, OH, COOH, and nullC(O)R9; R9 is hydrogen or a monovalent saturated or unsaturated aliphatic hydrocarbyl moiety.
摘要翻译：公开了包含用于抑制革兰氏阳性细菌产生外来蛋白的芳族化合物的组合物。本发明的芳族抑制化合物具有以下通式：其中R1选自H，-OR5，-R6C（O）H，-R6OH，-R6COOH，-OR6OH，-OR6COOH，-C（O ）NH 2和NH 2及其盐; R5是单价饱和或不饱和脂族烃基部分; R6是二价饱和或不饱和脂族烃基部分; R7是三价饱和或不饱和脂族烃基部分; R8是单价取代或未取代的饱和或不饱和脂族烃基部分，其可以或不会被杂原子中断; R 2，R 3和R 4独立地选自H，OH，COOH和-C（O）R 9; R9是氢或一价饱和或不饱和脂族烃基部分。

86. 发明申请

US20030130343A1 Fat accumulation-modulating compounds 审中-公开
标题翻译：脂肪蓄积调节化合物
公开(公告)号：US20030130343A1
公开(公告)日：2003-07-10
申请号：US10216365
申请日：2002-08-08
申请人： AdipoGenix, Inc.
发明人： Michael John Stevenson , Harry Jefferson Leighton
IPC分类号： A61K031/36 , A61K031/24 , A61K031/195 , A61K031/165 , A61K031/18
CPC分类号： A61K31/165 , A61K31/18 , A61K31/195 , A61K31/24 , A61K31/36 , A61K31/42 , A61K31/44
摘要： The present invention pertains to compounds effective at modulating fatty acid or triglyceride accumulation by fat cells, such compounds having therapeutic potential as regulators of body mass and for the treatment of overweight individuals, obesity, and metabolic disorders. Featured compounds are those having the structure set forth and exemplified herein: 1 wherein Ar is a substituted or unsubstituted phenyl group; R is a hydrogen or C1-6 alkyl group; and P is a substituted or unsubstituted nitrogen-containing heteroaryl group; said compound having the property of modulating the accumulation of fatty acids by cells. Therapeutic methods and pharmaceutical compositions featuring these compounds are also provided.
摘要翻译：本发明涉及有效调节脂肪细胞脂肪酸或甘油三酯积累的化合物，具有治疗潜力的化合物作为体重调节剂和治疗超重个体，肥胖症和代谢紊乱。特征化合物是具有本文列举和示例的结构的化合物：其中Ar是取代或未取代的苯基; R是氢或C 1-6烷基; 并且P是取代或未取代的含氮杂芳基; 所述化合物具有调节细胞积累的脂肪酸的性质。还提供了具有这些化合物的治疗方法和药物组合物。

87. 发明申请

US20030124177A1 Compositions and methods for transdermal oxybutynin therapy 审中-公开
标题翻译：透皮奥昔布宁治疗的组合物和方法
公开(公告)号：US20030124177A1
公开(公告)日：2003-07-03
申请号：US10286346
申请日：2002-11-01
申请人： Watson Pharmaceuticals, Inc.
发明人： Charles D. Ebert , Steven W. Sanders
IPC分类号： A61K009/70 , A61K031/24
CPC分类号： A61K9/7061 , A61K9/0014 , A61K9/0024 , A61K9/1647 , A61K31/216 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
摘要： The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder.
摘要翻译：本发明提供了用于奥昔布宁的组合物和方法，同时最小化与奥昔布宁治疗相关的不良药物经历的发生率和/或严重程度。在一个方面，这些组合物和方法提供了较低的奥昔布宁代谢物的血浆浓度，例如N-去乙氧基丁啶，其被推定为至少部分地促成一些不良药物经历，同时保持足够的奥昔布宁血浆浓度以有益于奥昔布宁治疗。本发明还提供了符合以下特征的奥昔布宁及其代谢物的异构体，这些特征使不良药物经历的发生率和/或严重程度最小化，以及维持膀胱过度活动症的有益和有效治疗。

88. 发明申请

US20030124174A1 Method for treating non-neuropathic pain 审中-公开
标题翻译：治疗非神经性疼痛的方法
公开(公告)号：US20030124174A1
公开(公告)日：2003-07-03
申请号：US10045341
申请日：2001-10-25
申请人： Endo Pharmaceuticals, Inc
发明人： Bradley Stuart Galer
IPC分类号： A61K009/70 , A61K031/24
CPC分类号： A61K9/7023 , A61K31/167
摘要： A method including topically administering an effective amount of local anesthetic to a patient is disclosed. The method is effective for inducing analgesia for treating non-neuropathic pain. Non-neuropathic pain suitable for treatment according to the invention includes pain associated with sports injuries; sprains; strains; soft-tissue injury; repetitive motion injury; carpal tunnel syndrome; injury to tendons, ligament, and muscles; conditions such as fibromyalgia, bursitis, castrochondritis, myofascial pain, and pain associated with arthritis, inflammation, contusions, post-surgical pain, and nociceptive pain. Preferably, the lidocaine is applied via a transdermal patch applied near the locus of pain.
摘要翻译：公开了一种包括向患者局部施用有效量的局部麻醉剂的方法。该方法对于诱导止痛治疗非神经性疼痛是有效的。适用于根据本发明治疗的非神经性疼痛包括与运动损伤相关的疼痛; 扭伤菌株软组织损伤; 重复性运动损伤; 腕管综合症; 对肌腱，韧带和肌肉的损伤; 诸如纤维肌痛，滑囊炎，硬骨炎，肌筋膜疼痛和与关节炎相关的疼痛，炎症，挫伤，手术后疼痛和伤害性疼痛等疾病。优选地，利多卡因通过施加在疼痛位置附近的透皮贴剂施用。

89. 发明申请

US20030108496A1 Compositions comprising phenyl-glycine derivatives 有权
标题翻译：包含苯基 - 甘氨酸衍生物的组合物
公开(公告)号：US20030108496A1
公开(公告)日：2003-06-12
申请号：US10294741
申请日：2002-11-15
发明人： Ruey J. Yu , Eugene J. Van Scott
IPC分类号： A61K031/7048 , A61K031/7008 , A61K031/24 , A61K031/16 , A61K031/198 , A61K007/42
CPC分类号： A61Q3/00 , A61K8/44 , A61K31/19 , A61K31/198 , A61K31/205 , A61K31/223 , A61K45/06 , A61Q5/00 , A61Q5/006 , A61Q19/00 , A61Q19/08 , A61K2300/00
摘要： The invention relates to compositions and methods useful for treating a variety of cosmetic conditions and dermatological disorders, where the composition includes a phenyl glycine derivative represented by the following formula: 1 wherein, R1 and R2 are independently H, I, F, Cl, Br, OH, SH, NH2, NHNH2, alkyl, aralkyl, alkoxy, acetoxy, acyloxy group having 1 to 9 carbon atoms, and being attached at the 2, 3 or 4 position of the phenyl group, whereby when R1 and/or R2 are OH, SH, NH2, they may be acetylated or acylated with 1 to 9 carbon atoms; R3 is H, formyl, acetyl, propanoyl, acyl, alkyl, aralkyl or an aryl group having 1 to 9 carbon atoms; R4 is OH, NH2, NHOH, NHNH2, or OR; where R is an alkyl, aralkyl or aryl group having 1 to 9 carbon atoms; the H attached to any carbon or nitrogen atom may be substituted by I, F, Cl, Br, OH, SH, NH2, NHNH2, an alkyl, aralkyl, alkoxy or acyl group having 1 to 9 carbon atoms. Phenyl-glycine and its derivatives may be present as isomeric D or L, non-isomeric or racemic DL, as a free acid, salt, lactone, amide or ester form.
摘要翻译：本发明涉及可用于治疗各种美容条件和皮肤疾病的组合物和方法，其中组合物包含由下式表示的苯基甘氨酸衍生物：其中，R 1和R 2独立地为H，I，F，Cl，Br， OH，SH，NH 2，NHNH 2，烷基，芳烷基，烷氧基，乙酰氧基，具有1至9个碳原子的酰氧基，并且在苯基的2,3或4位上连接，由此当R 1和/或R 2为OH ，SH，NH 2，它们可以被1至9个碳原子乙酰化或酰化; R3是H，甲酰基，乙酰基，丙酰基，酰基，烷基，芳烷基或具有1至9个碳原子的芳基; R4是OH，NH2，NHOH，NHNH2或OR; 其中R是具有1至9个碳原子的烷基，芳烷基或芳基; 可以被I，F，Cl，Br，OH，SH，NH 2，NHNH 2，具有1至9个碳原子的烷基，芳烷基，烷氧基或酰基所取代的任何碳原子或氮原子上的H。苯基甘氨酸及其衍生物可以作为游离酸，盐，内酯，酰胺或酯形式存在为异构体D或L，非异构体或外消旋DL。

90. 发明申请

US20030100608A1 1,4-disubstituted benzo-fused cycloalkyl urea compounds 有权
标题翻译： 1,4-二取代苯并稠合环烷基脲化合物
公开(公告)号：US20030100608A1
公开(公告)日：2003-05-29
申请号：US10154535
申请日：2002-05-24
申请人： Boehringer Ingelheim Pharmaceuticals, Inc.
发明人： Pier Francesco Cirillo , Eugene R. Hickey
IPC分类号： A61K031/277 , A61K031/17 , A61K031/24 , C07C275/28
CPC分类号： C07D213/64 , C07D213/36 , C07D213/68 , C07D213/70 , C07D213/81 , C07D239/34 , C07D239/47 , C07D239/52 , C07D251/46 , C07D295/088 , C07D295/13 , C07D309/38 , C07D401/06
摘要： Disclosed are compounds of the formula (I) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds. 1 wherein n, X, A, L, J, p, Q, Y and z are described herein.
摘要翻译：公开了下述式（I）的化合物，其作为抗炎剂是有活性的。还公开了使用和制备这些化合物的方法。其中n，X，A，L，J，p，Q，Y和z在本文中描述。

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